Десмопрессин является синтетическим аналогом природного антидиуретического гормона аргинин-вазопрессина.
Структурные изменения в молекуле аргинин-вазопрессина (дезаминирование цистеина в положении 1 и замещение L-аргинина на D-аргинин в положении 8) обуславливают уменьшение вазопрессорной активности и усиление антидиуретического действия десмопрессина. Препарат увеличивает проницаемость эпителия дистальных отделов извитых канальцев почек для воды и повышает ее реабсорбцию. Применение десмопрессина приводит к уменьшению объема выделяемой мочи и одновременному повышению осмолярности мочи и снижению осмолярности плазмы крови. Это приводит к снижению частоты мочеиспусканий и уменьшению ночной полиурии.
Антидиуретическая активность проявляется через 15-30 минут после введения дозы, достигает клинически значимой в течение 1 ч и остается высокой в течение 8 ч после введения дозы.
Фармакокинетика
Биодоступность десмопрессина при интраназальном введении составляет около 10%.
После введения 20 мкг десмопрессин обнаруживается в плазме через 15 мин. Cmax после интраназального введения достигается через 1 ч. Десмопрессин связывается с белками в очень незначительной степени. Выводится с грудным молоком человека в низкой концентрации.
Десмопрессин, подобно вазопрессину, метаболизируется в основном в печени и почках. Однако, дезаминирование цистеина-1 придает ему устойчивость к ферментативному распаду, что выражается в значительно более продолжительном T1/2 десмопрессина. T1/2 составляет около 4 ч. Не имеется сведений об энтеропеченочной циркуляции и о фармакологической активности его метаболитов.
Показания к применению
несахарный диабет центрального генеза;
первичный ночной энурез у детей 5 лет и старше;
диагностический тест на концентрационную способность почек.
декомпенсированная сердечная недостаточность (в т.ч. и в анамнезе);
необходимость применения терапии диуретиками;
гипонатриемия;
привычная полидипсия (врожденная или психогенная);
предрасположенность к тромбозам;
аллергический ринит;
заложенность носа;
отек и рубцовые изменения слизистой носа;
инфекции верхних дыхательных путей;
нарушение сознания;
повышенная чувствительность к компонентам препарата.
С осторожностью
С осторожностью следует применять препарат при почечной недостаточности, фиброзе мочевого пузыря, детям до 1 года и пожилым, при нарушениях водно-электролитного баланса, потенциальном риске повышения внутричерепного давления, во время беременности.
Применение при беременности и в период грудного вскармливания
Вазомирин следует назначать с осторожностью беременным пациенткам, несмотря на очень низкую активность десмопрессина в стимуляции родовой деятельности. Вредного воздействия десмопрессина на плод не выявлено.
Количество десмопрессина, которое может передаваться новорожденному с молоком матери, значительно меньше того, которое необходимо для влияния на диурез. Однако, рекомендуется проявлять осторожность при назначении лечения женщинам, кормящим грудью.
Способ применения и дозы
Препарат предназначен для интраназального введения.
Первичный ночной энурез
Начальная доза для детей (начиная с 5 лет) и для взрослых (до 65 лет), у которых имеется первичный ночной энурез, но с нормальной концентрационной способностью почек, составляет 20 мкг - одно нажатие на дозирующее устройство (10 мкг) в каждый носовой ход на ночь перед сном.
При необходимости дозу следует увеличить до 40 мкг - два нажатия на дозирующее устройство (20 мкг) в каждый носовой ход.
Решение о продолжении лечения принимается через 3 месяца непрерывной терапии на основании клинических данных, которые будут наблюдаться после отмены препарата в течение одной недели.
В случае лечения энуреза, прием жидкости должен быть ограничен до минимума - только для утоления жажды за 1 ч до и в течение 8 ч после введения препарата.
Несахарный диабет центрального генеза
Доза подбирается индивидуально, однако, как показывает клинический опыт, средняя суточная доза у взрослых составляет 10-40 мкг, у детей - 10-20 мкг (одно или два нажатия на дозирующее устройство (10-20 мкг) 1 или 2 раза в сутки. Эта суточная доза может даваться однократно или может быть разделена на 2-3 приема.
Тест на концентрационную способность почек
Для определения концентрационной способности почек используются следующие средние дозы: для взрослых - 40 мкг; детей старше 1 года - 10-20 мкг, детей в возрасте до 1 года -10 мкг.
Сразу после введения препарата пациенту необходимо опорожнить мочевой пузырь и на время проведения теста и 4 часа после его окончания применения (всего 8 часов) отбирается 2 порции мочи для измерения ее осмоляльности. Во время теста необходимо ограничить прием жидкости (объем жидкости, поступившей в организм за 1 ч до исследования и в течение 8 ч после не должен превышать 0.5 л).
Для большинства пациентов нормальным показателем осмоляльности мочи после назначения Вазомирина является 800 мОсм/кг. У детей концентрация мочи 600 мОсм/кг должна достигаться в течение 5 ч после введения препарата. Если выявлен показатель осмоляльности ниже этого значения, то исследование следует повторить. Повторное выявление низкого значения свидетельствует о нарушении концентрационной способности почек, и в этом случае пациент нуждается в дополнительном обследовании.
Побочное действие
Могут наблюдаться: головная боль, боль в животе, тошнота, отек слизистой оболочки носа, ринит и носовое кровотечение. В редких случаях наблюдаются аллергические реакции на компоненты препарата в виде кожных проявлений.
В единичных случаях - головокружение, повышение артериального давления, альгодисменорея, коньюктивит, снижение слезоотделения.
Лечение десмопрессином без одновременного снижения потребления жидкости может сопровождаться задержкой жидкости в организме, сопровождающейся гипонатриемией, повышением массы тела, отеками и в тяжелых случаях - преходящими неврологическими нарушениями, в основном, генерализованными судорогами.
Взаимодействие с другими лекарственными средствами
Индометацин может усиливать, но не увеличивать продолжительность действия десмопрессина.
Пероральные гипогликемические средства, например, глибенкламид, могут уменьшать продолжительность действия десмопрессина.
Терапия в сочетании с лекарственными средствами, которые вызывают высвобождение антидиуретического гормона и усиливают антидиуретическую активность или нарушают водно-электролитный баланс, например, трициклические антидепрессанты (хлорпромазин и карбамазепин), клофибрат и хлорпропамид, усиливает антидиуретический эффект и увеличивает риск задержки жидкости в организме.
Необходимо проявлять особую осторожность в отношении пациентов с риском внутричерепной гипертензии; пациентов с нарушением водного и/или электролитного баланса и пациентов с нарушениями, при которых гипергидратация организма может представлять опасность, например, нарушение функции почек, сердечная недостаточность, муковисцидоз или проведение анестезии.
Перед назначением препарата Вазомирин следует исключить диагнозы психогенной полидипсии и алкоголизм.
Тест на концентрационную способность почек у детей в возрасте до 1 года должен выполняться только в условиях стационара.
Пациенты, получающие лечение в связи с первичным ночным энурезом, должны быть предупреждены о необходимости избегать чрезмерного потребления жидкости и о необходимости прекращения приема препарата Вазомирин в случае возникновения рвоты и/или диареи до восстановления у них нормального баланса жидкости в организме.
Для предупреждения задержки жидкости необходимо проявлять осторожность после проведения диагностических тестов по выявлению несахарного диабета или исследования концентрационной способности почек. Не следует форсировать введение жидкости ни перорально, ни парентерально, а пациенты должны принимать столько жидкости, сколько им требуется для утоления жажды.
Не следует применять Вазомирин при изменениях слизистой, таких как рубцы, отек или другие заболевания, так как это может привести к неравномерной и ненадежной абсорбции.
У пациентов с назальными нарушениями, включая простудные заболевания, существует риск неустойчивой и/или сниженной эффективности лекарственного препарата. Это также может наблюдаться и у пациентов, занимающихся таким видом деятельности, при котором лекарственное средство может удаляться из полости носа до его всасывания, например, при плавании.
Препарат Вазомирин не следует назначать детям, которым требуются дозы меньше 10 мкг десмопрессина (в форме ацетата гидрата).
Влияние на способность управления автомобилем и работы с механизмами
Прием препарата не оказывает отрицательного воздействия на способность управлять автомобилем и другими механизмами.
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свойства","slug":"pharmacologic_effects","body":[{"type":"paragraph","data":{"text":"Десмопрессин является синтетическим аналогом природного антидиуретического гормона аргинин-вазопрессина."}},{"type":"paragraph","data":{"text":"Структурные изменения в молекуле аргинин-вазопрессина (дезаминирование цистеина в положении 1 и замещение L-аргинина на D-аргинин в положении 8) обуславливают уменьшение вазопрессорной активности и усиление антидиуретического действия десмопрессина. Препарат увеличивает проницаемость эпителия дистальных отделов извитых канальцев почек для воды и повышает ее реабсорбцию. Применение десмопрессина приводит к уменьшению объема выделяемой мочи и одновременному повышению осмолярности мочи и снижению осмолярности плазмы крови. Это приводит к снижению частоты мочеиспусканий и уменьшению ночной полиурии."}},{"type":"paragraph","data":{"text":"Антидиуретическая активность проявляется через 15-30 минут после введения дозы, достигает клинически значимой в течение 1 ч и остается высокой в течение 8 ч после введения дозы."}},{"type":"header","data":{"text":"Фармакокинетика","level":4}},{"type":"paragraph","data":{"text":"Биодоступность десмопрессина при интраназальном введении составляет около 10%."}},{"type":"paragraph","data":{"text":"После введения 20 мкг десмопрессин обнаруживается в плазме через 15 мин. C\u003csub\u003emax\u003c/sub\u003e после интраназального введения достигается через 1 ч. Десмопрессин связывается с белками в очень незначительной степени. Выводится с грудным молоком человека в низкой концентрации."}},{"type":"paragraph","data":{"text":"Десмопрессин, подобно вазопрессину, метаболизируется в основном в печени и почках. Однако, дезаминирование цистеина-1 придает ему устойчивость к ферментативному распаду, что выражается в значительно более продолжительном T\u003csub\u003e1/2\u003c/sub\u003e десмопрессина. T\u003csub\u003e1/2\u003c/sub\u003e составляет около 4 ч. Не имеется сведений об энтеропеченочной циркуляции и о фармакологической активности его метаболитов."}}]},{"id":8,"name":"Показания к применению","slug":"indications","body":[{"type":"list","data":{"style":"ordered","items":["несахарный диабет центрального генеза;","первичный ночной энурез у детей 5 лет и старше;","диагностический тест на концентрационную способность почек."]}}]},{"id":9,"name":"Противопоказания","slug":"contraindications","body":[{"type":"list","data":{"style":"ordered","items":["анурия;","отечный синдром различного генеза;","синдром неадекватной секреции антидиуретического гормона;","гипоосмолярность плазмы;","декомпенсированная сердечная недостаточность (в т.ч. и в анамнезе);","необходимость применения терапии диуретиками;","гипонатриемия;","привычная полидипсия (врожденная или психогенная);","предрасположенность к тромбозам;","аллергический ринит;","заложенность носа;","отек и рубцовые изменения слизистой носа;","инфекции верхних дыхательных путей;","нарушение сознания;","повышенная чувствительность к компонентам препарата."]}}]},{"id":10,"name":"С осторожностью","slug":"cautions","body":[{"type":"paragraph","data":{"text":"\u003ci\u003eС осторожностью\u003c/i\u003e следует применять препарат при почечной недостаточности, фиброзе мочевого пузыря, детям до 1 года и пожилым, при нарушениях водно-электролитного баланса, потенциальном риске повышения внутричерепного давления, во время беременности."}}]},{"id":11,"name":"Применение при беременности и в период грудного вскармливания","slug":"pregnancy_warnings","body":[{"type":"paragraph","data":{"text":"Вазомирин следует назначать с осторожностью беременным пациенткам, несмотря на очень низкую активность десмопрессина в стимуляции родовой деятельности. Вредного воздействия десмопрессина на плод не выявлено."}},{"type":"paragraph","data":{"text":"Количество десмопрессина, которое может передаваться новорожденному с молоком матери, значительно меньше того, которое необходимо для влияния на диурез. Однако, рекомендуется проявлять осторожность при назначении лечения женщинам, кормящим грудью."}}]},{"id":12,"name":"Способ применения и дозы","slug":"dosage","body":[{"type":"paragraph","data":{"text":"Препарат предназначен для интраназального введения."}},{"type":"paragraph","data":{"text":"\u003ci\u003eПервичный ночной энурез\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Начальная доза для \u003cb\u003eдетей (начиная с 5 лет)\u003c/b\u003e и для \u003cb\u003eвзрослых (до 65 лет),\u003c/b\u003e у которых имеется первичный ночной энурез, но с нормальной концентрационной способностью почек, составляет 20 мкг - одно нажатие на дозирующее устройство (10 мкг) в каждый носовой ход на ночь перед сном."}},{"type":"paragraph","data":{"text":"При необходимости дозу следует увеличить до 40 мкг - два нажатия на дозирующее устройство (20 мкг) в каждый носовой ход."}},{"type":"paragraph","data":{"text":"Решение о продолжении лечения принимается через 3 месяца непрерывной терапии на основании клинических данных, которые будут наблюдаться после отмены препарата в течение одной недели."}},{"type":"paragraph","data":{"text":"В случае лечения энуреза, прием жидкости должен быть ограничен до минимума - только для утоления жажды за 1 ч до и в течение 8 ч после введения препарата."}},{"type":"paragraph","data":{"text":"\u003ci\u003eНесахарный диабет центрального генеза\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Доза подбирается индивидуально, однако, как показывает клинический опыт, средняя суточная доза у \u003cb\u003eвзрослых\u003c/b\u003e составляет 10-40 мкг, у \u003cb\u003eдетей \u003c/b\u003e- 10-20 мкг (одно или два нажатия на дозирующее устройство (10-20 мкг) 1 или 2 раза в сутки. Эта суточная доза может даваться однократно или может быть разделена на 2-3 приема."}},{"type":"paragraph","data":{"text":"\u003ci\u003eТест на концентрационную способность почек\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Для определения концентрационной способности почек используются следующие средние дозы: для \u003cb\u003eвзрослых\u003c/b\u003e - 40 мкг; \u003cb\u003eдетей старше 1 года\u003c/b\u003e - 10-20 мкг, \u003cb\u003eдетей в возрасте до 1 года\u003c/b\u003e -10 мкг."}},{"type":"paragraph","data":{"text":"Сразу после введения препарата пациенту необходимо опорожнить мочевой пузырь и на время проведения теста и 4 часа после его окончания применения (всего 8 часов) отбирается 2 порции мочи для измерения ее осмоляльности. Во время теста необходимо ограничить прием жидкости (объем жидкости, поступившей в организм за 1 ч до исследования и в течение 8 ч после не должен превышать 0.5 л)."}},{"type":"paragraph","data":{"text":"Для большинства пациентов нормальным показателем осмоляльности мочи после назначения Вазомирина является 800 мОсм/кг. У детей концентрация мочи 600 мОсм/кг должна достигаться в течение 5 ч после введения препарата. Если выявлен показатель осмоляльности ниже этого значения, то исследование следует повторить. Повторное выявление низкого значения свидетельствует о нарушении концентрационной способности почек, и в этом случае пациент нуждается в дополнительном обследовании."}}]},{"id":13,"name":"Побочное действие","slug":"side_effects","body":[{"type":"paragraph","data":{"text":"Могут наблюдаться: головная боль, боль в животе, тошнота, отек слизистой оболочки носа, ринит и носовое кровотечение. В редких случаях наблюдаются аллергические реакции на компоненты препарата в виде кожных проявлений."}},{"type":"paragraph","data":{"text":"В единичных случаях - головокружение, повышение артериального давления, альгодисменорея, коньюктивит, снижение слезоотделения."}},{"type":"paragraph","data":{"text":"Лечение десмопрессином без одновременного снижения потребления жидкости может сопровождаться задержкой жидкости в организме, сопровождающейся гипонатриемией, повышением массы тела, отеками и в тяжелых случаях - преходящими неврологическими нарушениями, в основном, генерализованными судорогами."}}]},{"id":15,"name":"Взаимодействие с другими лекарственными средствами","slug":"drugs_interaction","body":[{"type":"paragraph","data":{"text":"Индометацин может усиливать, но не увеличивать продолжительность действия десмопрессина."}},{"type":"paragraph","data":{"text":"Пероральные гипогликемические средства, например, глибенкламид, могут уменьшать продолжительность действия десмопрессина."}},{"type":"paragraph","data":{"text":"Терапия в сочетании с лекарственными средствами, которые вызывают высвобождение антидиуретического гормона и усиливают антидиуретическую активность или нарушают водно-электролитный баланс, например, трициклические антидепрессанты (хлорпромазин и карбамазепин), клофибрат и хлорпропамид, усиливает антидиуретический эффект и увеличивает риск задержки жидкости в организме."}},{"type":"paragraph","data":{"text":"Глибутид, тетрациклин, литий, норэпинефрин ослабляют антидиуретическое действие. Десмопрессин усиливает действие гипертензивных средств."}}]},{"id":16,"name":"Особые указания","slug":"","body":[{"type":"paragraph","data":{"text":"Необходимо проявлять особую осторожность в отношении пациентов с риском внутричерепной гипертензии; пациентов с нарушением водного и/или электролитного баланса и пациентов с нарушениями, при которых гипергидратация организма может представлять опасность, например, нарушение функции почек, сердечная недостаточность, муковисцидоз или проведение анестезии."}},{"type":"paragraph","data":{"text":"Перед назначением препарата Вазомирин следует исключить диагнозы психогенной полидипсии и алкоголизм."}},{"type":"paragraph","data":{"text":"Тест на концентрационную способность почек у детей в возрасте до 1 года должен выполняться только в условиях стационара."}},{"type":"paragraph","data":{"text":"Пациенты, получающие лечение в связи с первичным ночным энурезом, должны быть предупреждены о необходимости избегать чрезмерного потребления жидкости и о необходимости прекращения приема препарата Вазомирин в случае возникновения рвоты и/или диареи до восстановления у них нормального баланса жидкости в организме."}},{"type":"paragraph","data":{"text":"Для предупреждения задержки жидкости необходимо проявлять осторожность после проведения диагностических тестов по выявлению несахарного диабета или исследования концентрационной способности почек. Не следует форсировать введение жидкости ни перорально, ни парентерально, а пациенты должны принимать столько жидкости, сколько им требуется для утоления жажды."}},{"type":"paragraph","data":{"text":"Не следует применять Вазомирин при изменениях слизистой, таких как рубцы, отек или другие заболевания, так как это может привести к неравномерной и ненадежной абсорбции."}},{"type":"paragraph","data":{"text":"У пациентов с назальными нарушениями, включая простудные заболевания, существует риск неустойчивой и/или сниженной эффективности лекарственного препарата. Это также может наблюдаться и у пациентов, занимающихся таким видом деятельности, при котором лекарственное средство может удаляться из полости носа до его всасывания, например, при плавании."}},{"type":"paragraph","data":{"text":"Препарат Вазомирин не следует назначать детям, которым требуются дозы меньше 10 мкг десмопрессина (в форме ацетата гидрата)."}},{"type":"paragraph","data":{"text":"\u003ci\u003eВлияние на способность управления автомобилем и работы с механизмами\u003c/i\u003e"}},{"type":"paragraph","data":{"text":"Прием препарата не оказывает отрицательного воздействия на способность управлять автомобилем и другими механизмами."}}]}],"source":null},"description_toggle":false,"short_description":"Десмопрессин является синтетическим аналогом природного антидиуретического гормона аргинин-вазопрессина. 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